Endothelin-2, human

A peptide vasoconstrictor

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货号: ajce56216
CAS: 123562-20-9
别名: 内皮素2,Endothelin-2 (human, canine); Human endothelin-2
分子式: C115H160N26O32S4
分子量: 2546.92
纯度: >98%
溶解度: Soluble in DMSO
储存: Store at -20°C
库存: 现货

Background

Endothelin-2 is a peptide vasoconstrictor and ligand for the endothelin (ET) receptors ET_A and ET_B (K_bs= 32.8 and 1.33 nM, respectively).¹ It induces β-arrestin recruitment in CHO-K1 cells expressing human ET_A and ET_B (pD₂s =8.75 and 8.55, respectively). Ex vivo, endothelin-2 induces vformal asoconstriction in isolated rat mesenteric arterial beds (ED₅₀ = 90.8 pmol).² Endothelin-2 also induces contraction of isolated rat uteri, an effect which is reversed by the ET_A antagonist BQ-123 but not the ET_B antagonist BQ-788 .³ Infusion of endothelin-2 restores vasoconstriction of vessels at the follicular apex of the ovarian follicle and ovulation in Amhr2^cre/+Smo2 mice.⁴

1.Maguire, J.J., Kuc, R.E., Pell, V.R., et al.Comparison of human ETA and ETB receptor signalling via G-protein and β-arrestin pathwaysLife Sci.91(13-14)544-549(2012) 2.Douglas, S.A., and Hiley, C.R.Endothelium-dependent vascular activities of endothelin-like peptides in the isolated superior mesenteric arterial bed of the ratBr. J. Pharmacol.101(1)81-88(1990) 3.Kousides, M., Story, M.E., and Pennefather, J.N.Endopeptidase 24.11 inhibition does not modify uterotonic effects of endothelins in rat uterusPeptides19(9)1585-1593(1998) 4.Migone, F.F., Cowan, R.G., Williams, R.M., et al.In vivo imaging reveals an essential role of vasoconstriction in rupture of the ovarian follicle at ovulationProc. Natl. Acad. Sci. USA113(8)2294-2299(2016)

Protocol

Animal experiment:

Rats[1]For the assay of pressor activity, male Wistar rats weighing 300-350 g are anesthetized with urethane (1 g/kg i.p.) and pretreated with atropine (0.25 mg/kg i.v.), propranolol (1 mg/kg i.v.), and bunazocine (1 mg/kg i.v.). Additional maintenance doses (one-half of the initial doses) of the autonomic blockades are administered every 3-4 hr. Each animal is given only one bolus of Endothelin-2. 1 nM of Endothelin-2 in 50 μL of buffer is bolus injected from a cannula inserted in the right femoral vein. The blood pressure is recorded from a cannula, which is placed in the right carotid artery and connected to a pressure transducer[1].

参考文献:

[1]. Grimshaw MJ, et al. Endothelin-2 is a macrophage chemoattractant: implications for macrophage distribution in tumors. Eur J Immunol. 2002 Sep;32(9):2393-400.